Anti Parkinson Drugs Flashcards

1
Q

Anti cholinergic drugs bykhlasu keln b —– ma 3ada——

A

Hydrochloride
Mesylate

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2
Q

Agents that increase dopamine synthesis:
Levodopa:
Transported — to CNs
Converted to dopamine in —-
Only —-% of L dopa reaches the brain

A

Actively
Brain
1-3

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3
Q

Side effects of levodopa:
1-
2-
3-
4-

A

1-GI irritation and stimulation of CTZ
2-Upset stomach with nausea and vomiting
3-dyskinesia (involuntary movements)(overactivity of dopamine receptors)
4-mood changes,depression and psychosis

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4
Q

Agents that increase dopamine synthesis:
Dopamine:
Lower doses—-
High doses——
D1 and D2 in——
Effect of binding to D1 nad D2:
Dopamine is metabolized to —– by MAO or COMT

A

Vasoconstriction on alpha
Stimulates B1 cardiac receptors
Perioheral mesenteric and renal
Vasodlation
Homoooosexua(azde homovanillic acid)

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5
Q

How to increase levodopa in brain?

A

By carbidopa
Its a decarboxylase inhibitor that prevents metabolization of dopamine in the periphery so more levodopa will reach the brain (10%) and decrease the required levodopa by 5 times

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6
Q

T or F
Carbidopa cross the BBB

A

Falseee zaddy
Acts peripherally

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7
Q

T or F
Pyridoxine (B6) decrease the breakdown of levodopa in the oeriohery

A

Ghalaaaaaat
Bl aakesss
Byshtghl b 3aks l bestie carbidopa

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8
Q

T or f
Administration of MAO inhibitors with levodopa can lead to hypertensive crisis

A

Ehhhhh wley

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9
Q

Agents that inhibit dopamine metabolism
MAO inhibitors
1-
2-
Reversible or rrieversible inhibition?

A

Khaletna giline
Selegiline
Rasagiline 2nd generation
Irrreeeeeeversible

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10
Q

T or F
COMt trasforms normetadrenaline to VMA
And MAO converts noradrenaline to normetadrenaline

A

Falseeee
Reverseddd

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11
Q

Khaletna giline is —— administered and —- metabolized
Selegiline bser —– then will lead to —- and ——-
Rasagiline bser ——

A

Orally
Extensively
Amphetamine
Insomnia and vasoconstriction
1-aminoindan ma eendu vasoactive effect

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12
Q

T or F
Rasagilineee is selective for MAO type A

A

False
Type B

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13
Q

Agents that inhibit dopamine metabolism
COMT inhibitors
Khaletna —–
Whde m—–w whde m—-
Reversible or itreversible?

A

Caponeeeee
Whde Tolcapone w whde entacapone
Reversible

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14
Q

COMt transform dopamine to —–
Thus inhibiting it will —-

A

3 O methyl dopa
Prolong its effect

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15
Q

Inhibition of dopamine metabolism by carbidopa will lead to its metabolism by COMT to ——
This molecule will consequentially —— with —— thus—-
So entacapone is administered to ——

A

3 o methyl dopa
Compete with levodopa on the active tranport sites
Thus diminish its activity
Reduce methyl o dopa plasma levels by inhibiting COMt

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16
Q

T or F
Entacapone have longer effects than tolcapone
Entacapone acts mostly in the periphery while tolcapone acts centrally and peripherally

A

False
Tolcapone 8-12 hr
Entacapine 2 hr

17
Q

Side effects of khalte capone:
1-
2-

A

Nausea
Hallucinations

18
Q

Fatal hepatic failure occurs only with entacapone

A

Falseee
With tolcapone

19
Q

Stalevo composition:

A

12.5 mg carbidopa
50 mg of levodopa
200 mg entacapone

20
Q

Agents that increase dopamine release
1-
Mode of action
Entery and excretion
More potent or less than levodopa
Adverse effects
1-
2-
3-
4-

A

Amantadine (mantadix)
Increase dopamine release from neurons and inhibit dopamine reuptake
Lipophilic that may enter the brain
Unchanged renal excretion
Less potent than levodopa
1-insomnia
2-hallucination
3-depression
4-confusion and agitation

21
Q

Dopamine receptor agonists:
Duration of action:
Risk of dyskinesia:
Type of receptors:
Adverse:

A

Longerrrr than levodopa
Less than levodopa
D2
Nausea,vomiting and hallucinations

22
Q

Bromocriptine
Derivative of ——
Full agonist at ——-
At low doses used for—
High doses
Dyskinesia?
Adverse effects
Hepatic metabolism metabolism
T1/2

A

Vasoconstrictive ergotamine
D2
Hperprolactinemia
For parkinson
Less prominent
Same as levo plus serious cardiac problems with patients with MI
Worsening of vasospasm (alpha1 agonist)
90% undergo hepatic metabolism
3hr

23
Q

Ropinirole and pramipexole
Ergot?
Receptors?
Exacerbate vasospasm?

A

No
D2 and D3
No

24
Q

Ripinirole
—– active and metabolized by — with half life —– dyskinesia is —— frequent than in levodopa
Pramipexole
——- absorbed
Eliminated via—–
Half life

A

Orally
Cyp1A2
6hrs
Orally
Unchangeddddd via kidney
8-12 hrs

25
Q

Rotigotine
Receptors
Ergot?
Usages
Mode of administration

A

D1 D2 D3
No
Earlytt stage of parkinson
Once daily trandermal patch (24hr)

26
Q

Apomorphine
Kef byaamlu?
Receptorsv
Orally or IV?
Usage
Duration of action

A

Morphine with boiling acid
D1 and D2
Subcutaneous mwah
Late stage of parkinson
45-90 min

27
Q

T or F
Apomorphine have emetic effects like dopamine

A

Truee